BRD2
BRD2 is a BET-family epigenetic reader with tandem bromodomains that bind lysine-acetylated histones and transcription factors, recruit transcription factors and coactivators, and support RNA polymerase II-dependent transcriptional elongation[1]. Mechanistically, BET proteins including BRD2, BRD3, BRD4, and BRDT connect acetylated chromatin to gene-expression programs that regulate transcription, chromatin remodeling, DNA replication, and DNA damage repair[1]. In pancreatic β-cells, BET inhibition with JQ1 increased insulin secretion and insulin content, while specific inhibition of Brd2 increased fatty acid oxidation, showing a discrete metabolic role for BRD2 compared with other BET isoforms[2]. Compared with BRD4, BRD2 appears less dominant in several disease models: BRD4, not BRD2 or BRD3, increased after repeated cocaine exposure, and BRD4 was preferentially linked to cocaine-induced Bdnf expression[3]. In prostate cancer, BET proteins BRD2, BRD3, and BRD4 are stabilized by SPOP mutations, contributing to BET-inhibitor resistance, but BRD4 often carries the main disease-specific transcriptional signal[4]. For experimental applications, pan-BET inhibitors such as JQ1, I-BET, OTX015, and RVX-208 help probe BRD2-containing acetyl-lysine reader complexes, although their limited isoform selectivity requires paired genetic approaches for BRD2-specific interpretation[5].
References:
- [1]. Cheung KL, et al. The Functions of BET Proteins in Gene Transcription of Biology and Diseases. Front Mol Biosci. 2021 Sep 3;8:728777. [Content Brief]
- [2]. Deeney JT, et al. BET Bromodomain Proteins Brd2, Brd3 and Brd4 Selectively Regulate Metabolic Pathways in the Pancreatic β-Cell. PLoS One. 2016 Mar 23;11(3):e0151329. [Content Brief]
- [3]. Sartor GC, et al. Epigenetic Readers of Lysine Acetylation Regulate Cocaine-Induced Plasticity. J Neurosci. 2015 Nov 11;35(45):15062-72. [Content Brief]
- [4]. Dai X, et al. Prostate cancer-associated SPOP mutations confer resistance to BET inhibitors through stabilization of BRD4. Nat Med. 2017 Sep;23(9):1063-1071. [Content Brief]
- [5]. Lucas X, et al. Targeting the BET family for the treatment of leukemia. Epigenomics. 2014 Apr;6(2):153-5. [Content Brief]
-
BRD2 Related Products (60)
Related Products (60)
-
Antibodies (1)
-
ABBV-744
0 ImagesABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.
-
GSK778
0 ImagesSynonyms: iBET-BD1GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
-
BBC0403
0 ImagesBBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research.
-
BET-IN-30
0 ImagesCat. No.: HY-181735BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML.
-
PROTAC BRD4 Degrader-46
0 ImagesCat. No.: HY-182801CAS No.: 2766179-68-2PROTAC BRD4 Degrader-46 is a heterobifunctional BRD4 PROTAC degrader. PROTAC BRD4 Degrader-46 binds to both BRD4 and CRBN, thereby triggering ubiquitination and proteasomal degradation of BRD4. PROTAC BRD4 Degrader-46 downregulates the levels of downstream BRD2, BRD3 and MYC. PROTAC BRD4 Degrader-46 can be used in the research of cancers such as multiple myeloma.
-
GSK046
0 ImagesSynonyms: iBET-BD2GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.
-
IBG3
0 ImagesCat. No.: HY-160528Purity: 98.53%IBG3 is a Molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia.
-
TMX1
0 ImagesTMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity.
-
IBG1
0 ImagesIBG1 is a molecular glue degrader targeting BRD2 and BRD4 (DC50: 0.15 nM). IBG1 has no significant degradation effect on its paralogue BRD3. IBG1 can inhibit the growth of cancer cells and can be used in tumor research. (Pink: BRD2/BRD4 Ligand (HY-111139); Black: Linker; Blue: DCAF15 ligand-1 (HY-W037495)).
-
GSK973
0 ImagesGSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
-
(S)-JQ-35
0 ImagesSynonyms: TEN-010(S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma.
-
HJB97
0 ImagesHJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
-
RVX-297
0 ImagesCat. No.: HY-114504CAS No.: 1044871-04-6RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
